Bepotastine is available as an ophthalmic solution and oral tablet. It is a direct H1-receptor antagonist that inhibits the release of histamine from mast cells.[2] The ophthalmic formulation has shown minimal systemic absorption, between 1 and 1.5% in healthy adults.[3] Common side effects are eye irritation, headache, unpleasant taste, and nasopharyngitis.[3] The main route of elimination is urinary excretion, 75-90% excreted unchanged.[3]
Marketing historyEdit
It is marketed in Japan by Tanabe Seiyaku under the brand name Talion. Talion was co-developed by Tanabe Seiyaku and Ube Industries, the latter of which discovered bepotastine. In 2001, Tanabe Seiyaku granted Senju, now owned by Allergan, exclusive worldwide rights, with the exception of certain Asian countries, to develop, manufacture and market bepotastine for ophthalmic use. Senju, in turn, has granted the United States rights for the ophthalmic preparation to ISTA Pharmaceuticals.
Sales and patentsEdit
In 2011, ISTA pharmaceuticals experienced a 2.4% increase in net revenues from 2010, which was driven by the sales of Bepreve. Their net revenue for 2011 was $160.3 million.[4]ISTA Pharmaceuticals was acquired by Bausch & Lomb in March 2012 for $500 million.[5] Bausch & Lomb hold the patent for bepotastine besilate (https://www.accessdata.fda.gov/scripts/cder/ob/docs/temptn.cfm. On November 26, 2014, Bausch & Lomb sued Micro Labs USA for patent infringement.[6] Bausch & Lomb was recently bought out by Valeant Pharmaceuticals in May 2013 for $8.57 billion, Valeant's largest acquisition to date, causing the company's stock to rise 25% when the deal was announced.[7]
Clinical trialsEdit
A Phase III clinical trial was carried out in 2010 to evaluate the effectiveness of bepotastine besilate ophthalmic solutions 1.0% and 1.5%.[8] These solutions were compared to a placebo and evaluated for their ability to reduce ocular itchiness. The study was carried out with 130 individuals and evaluated after 15 minutes, 8 hours, or 16 hours. There was a reduction in itchiness at all-time points for both ophthalmic solutions. The study concluded that bepotastine besilate ophthalmic formulations reduced ocular itchiness for at least 8 hours after dosing compared to placebo. Phase I and II trials were carried out in Japan.
Studies have been performed in animals and bepotastine besilate was not found to be teratogenic in rats during fetal development, even at 3,300 times more than typical use in humans.[3] Evidence of infertility was seen in rats at 33,000 times the typical ocular dose in humans.[3] The safety and efficacy has not been established in patients under 2 years of age and has been extrapolated from adults for patients under 10 years of age.[3]
ReferencesEdit
^Takahashi H, Ishida-Yamamoto A, Iizuka H (September 2004). "Effects of bepotastine, cetirizine, fexofenadine, and olopatadine on histamine-induced wheal-and flare-response, sedation, and psychomotor performance". Clinical and Experimental Dermatology. 29 (5): 526–32. doi:10.1111/j.1365-2230.2004.01618.x. PMID 15347340. S2CID 9843760.
^"2011 Net Revenues Increase to $160.3 Million On an Adjusted Cash Net Income Basis, ISTA Posts Second Year of Profitability Company Reaffirms 2012 Financial Guidance". Last 10K. February 23, 2012.
^"Bausch & Lomb to Buy ISTA Pharmaceuticals for $500 Million". DealBook. 26 March 2012. Retrieved 2015-12-05.
^"Bausch & Lomb Inc. et al. v. Micro Labs USA, Inc. et al". Patent Docs. JD Supra, LLC. December 8, 2014.
^Blackwell R, Silcoff S, Marotte B (27 May 2013). . The Globe and Mail. Archived from the original on 28 May 2013.
^Macejko TT, Bergmann MT, Williams JI, Gow JA, Gomes PJ, McNamara TR, Abelson MB (July 2010). "Multicenter clinical evaluation of bepotastine besilate ophthalmic solutions 1.0% and 1.5% to treat allergic conjunctivitis". American Journal of Ophthalmology. 150 (1): 122–127.e5. doi:10.1016/j.ajo.2010.02.007. PMID 20488431.
August 25, 2023
bepotastine, talion, bepreve, generation, antihistamine, approved, japan, treatment, allergic, rhinitis, urticaria, pruritus, july, 2000, january, 2002, respectively, marketed, united, states, drop, under, brand, name, bepreve, ista, pharmaceuticals, subsidiar. Bepotastine Talion Bepreve is a 2nd generation antihistamine 1 It was approved in Japan for use in the treatment of allergic rhinitis and urticaria pruritus in July 2000 and January 2002 respectively It is marketed in the United States as an eye drop under the brand name Bepreve by ISTA Pharmaceuticals a subsidiary of Bausch Lomb citation needed BepotastineClinical dataTrade namesBepreveAHFS Drugs comInternational Drug NamesMedlinePlusa610012Routes ofadministrationOral eye dropsATC codenoneLegal statusLegal statusCA only In general Prescription only Pharmacokinetic dataBioavailabilityHigh oral Minimal topical Protein binding 55 ExcretionRenal 75 85IdentifiersIUPAC name 4 4 4 chlorophenyl pyridin 2 ylmethoxy piperidin 1 yl butanoic acidCAS Number125602 71 3 NPubChem CID2350DrugBankDB04890 YChemSpider2260 YUNIIHYD2U48IASKEGGD09705 YChEBICHEBI 71204 NChEMBLChEMBL1201758 NCompTox Dashboard EPA DTXSID90904947Chemical and physical dataFormulaC 21H 25Cl N 2O 3Molar mass388 89 g mol 13D model JSmol Interactive imageSMILES Clc1ccc cc1 C OC2CCN CCCC O O CC2 c3ncccc3InChI InChI 1S C21H25ClN2O3 c22 17 8 6 16 7 9 17 21 19 4 1 2 12 23 19 27 18 10 14 24 15 11 18 13 3 5 20 25 26 h1 2 4 6 9 12 18 21H 3 5 10 11 13 15H2 H 25 26 YKey YWGDOWXRIALTES UHFFFAOYSA N Y N Y what is this verify Contents 1 Pharmacology 2 Marketing history 3 Sales and patents 4 Clinical trials 5 ReferencesPharmacology EditBepotastine is available as an ophthalmic solution and oral tablet It is a direct H1 receptor antagonist that inhibits the release of histamine from mast cells 2 The ophthalmic formulation has shown minimal systemic absorption between 1 and 1 5 in healthy adults 3 Common side effects are eye irritation headache unpleasant taste and nasopharyngitis 3 The main route of elimination is urinary excretion 75 90 excreted unchanged 3 Marketing history EditIt is marketed in Japan by Tanabe Seiyaku under the brand name Talion Talion was co developed by Tanabe Seiyaku and Ube Industries the latter of which discovered bepotastine In 2001 Tanabe Seiyaku granted Senju now owned by Allergan exclusive worldwide rights with the exception of certain Asian countries to develop manufacture and market bepotastine for ophthalmic use Senju in turn has granted the United States rights for the ophthalmic preparation to ISTA Pharmaceuticals Sales and patents EditIn 2011 ISTA pharmaceuticals experienced a 2 4 increase in net revenues from 2010 which was driven by the sales of Bepreve Their net revenue for 2011 was 160 3 million 4 ISTA Pharmaceuticals was acquired by Bausch amp Lomb in March 2012 for 500 million 5 Bausch amp Lomb hold the patent for bepotastine besilate https www accessdata fda gov scripts cder ob docs temptn cfm On November 26 2014 Bausch amp Lomb sued Micro Labs USA for patent infringement 6 Bausch amp Lomb was recently bought out by Valeant Pharmaceuticals in May 2013 for 8 57 billion Valeant s largest acquisition to date causing the company s stock to rise 25 when the deal was announced 7 Clinical trials EditA Phase III clinical trial was carried out in 2010 to evaluate the effectiveness of bepotastine besilate ophthalmic solutions 1 0 and 1 5 8 These solutions were compared to a placebo and evaluated for their ability to reduce ocular itchiness The study was carried out with 130 individuals and evaluated after 15 minutes 8 hours or 16 hours There was a reduction in itchiness at all time points for both ophthalmic solutions The study concluded that bepotastine besilate ophthalmic formulations reduced ocular itchiness for at least 8 hours after dosing compared to placebo Phase I and II trials were carried out in Japan Studies have been performed in animals and bepotastine besilate was not found to be teratogenic in rats during fetal development even at 3 300 times more than typical use in humans 3 Evidence of infertility was seen in rats at 33 000 times the typical ocular dose in humans 3 The safety and efficacy has not been established in patients under 2 years of age and has been extrapolated from adults for patients under 10 years of age 3 References Edit Takahashi H Ishida Yamamoto A Iizuka H September 2004 Effects of bepotastine cetirizine fexofenadine and olopatadine on histamine induced wheal and flare response sedation and psychomotor performance Clinical and Experimental Dermatology 29 5 526 32 doi 10 1111 j 1365 2230 2004 01618 x PMID 15347340 S2CID 9843760 Bepotastine Monograph Lexicomp a b c d e f Bepreve prescribing Information PDF 2011 Net Revenues Increase to 160 3 Million On an Adjusted Cash Net Income Basis ISTA Posts Second Year of Profitability Company Reaffirms 2012 Financial Guidance Last 10K February 23 2012 Bausch amp Lomb to Buy ISTA Pharmaceuticals for 500 Million DealBook 26 March 2012 Retrieved 2015 12 05 Bausch amp Lomb Inc et al v Micro Labs USA Inc et al Patent Docs JD Supra LLC December 8 2014 Blackwell R Silcoff S Marotte B 27 May 2013 Valenant pharmaceuticals eyes China with Bausch deal The Globe and Mail Archived from the original on 28 May 2013 Macejko TT Bergmann MT Williams JI Gow JA Gomes PJ McNamara TR Abelson MB July 2010 Multicenter clinical evaluation of bepotastine besilate ophthalmic solutions 1 0 and 1 5 to treat allergic conjunctivitis American Journal of Ophthalmology 150 1 122 127 e5 doi 10 1016 j ajo 2010 02 007 PMID 20488431 Retrieved from https en wikipedia org w index php title Bepotastine amp oldid 1171475930, wikipedia, wiki, book, books, library,
